Cisapride

Cisapride
Cisapride
Systematic (IUPAC) name
(±)-cis-4-amino-5-chloro-N-(1-[3-(4-fluorophenoxy)propyl]-3-methoxypiperidin-4-yl)-2-methoxybenzamide
Clinical data
Trade names Prepulsid, Propulsid
AHFS/Drugs.com FDA Professional Drug Information
MedlinePlus a694006
Pregnancy cat. B1 (Australia)
Legal status Schedule 4 (Australia)
Routes tablets, suspension
Pharmacokinetic data
Bioavailability 30-40%
Protein binding 97.5%
Metabolism hepatic, intestinal
Half-life 10 hours
Excretion renal, biliary
Identifiers
CAS number 81098-60-4 YesY
ATC code A03FA02
PubChem CID 2769
IUPHAR ligand 240
DrugBank APRD00454
ChemSpider 2667 YesY
UNII UVL329170W YesY
KEGG D00274 YesY
ChEMBL CHEMBL1729 N
Chemical data
Formula C23H29ClFN3O4 
Mol. mass 465.945 g/mol
SMILES eMolecules & PubChem
 N(what is this?)  (verify)

Cisapride is a gastroprokinetic agent, a drug which increases motility in the upper gastrointestinal tract. It acts directly as a serotonin 5-HT4 receptor agonist and indirectly as a parasympathomimetic. Stimulation of the serotonin receptors increases acetylcholine release in the enteric nervous system. It has been sold under the trade names Prepulsid (Janssen-Ortho) and Propulsid (in the U.S.). It was discovered by Janssen Pharmaceutica in 1980. In many countries, it has been either withdrawn from the market or had its indications limited because of side effects.

The commercial preparations of this drug are the racemic mixture of both enantiomers of the compound. The (+) enantiomer itself has the major pharmacologic effects and does not induce many of the detrimental side effects of the mixture.[1]

Contents

Clinical uses

Cisapride increases muscle tone in the esophageal sphincter in people with gastroesophageal reflux disease. It also increases gastric emptying in people with diabetic gastroparesis. It has been used to treat bowel constipation.

In many countries, it has been either withdrawn or had its indications limited because of reports of the side effect long QT syndrome, which predisposes to arrhythmias. The U.S. Food and Drug Administration (FDA) issued a warning letter to doctors,[2] and cisapride was voluntarily removed from the U.S. market on July 14, 2000.

Veterinary uses

Cisapride is still available in the United States for use in animals, and is commonly prescribed by veterinarians to treat megacolon in cats.

Cisapride is also commonly used to treat GI stasis in rabbits, sometimes in conjunction with metoclopramide (Reglan).

See also

References

  1. ^ US patent 5955478, Nancy M. Gray, N. M.; Young, J. W, "Methods for treating gastrointestinal motility dysfunction using optically pre (+) cisapride", issued 1999-Sep-21 
  2. ^ "Propulsid (cisapride) Safety Information". http://www.fda.gov/Safety/MedWatch/SafetyInformation/SafetyAlertsforHumanMedicalProducts/ucm175000.htm. Retrieved 2011-07-14. 

Sources

  • Brenner, G. M. (2000). Pharmacology. Philadelphia, PA: W.B. Saunders Company. ISBN 0-7216-7757-6
  • Canadian Pharmacists Association (2000). Compendium of Pharmaceuticals and Specialties (25th ed.). Toronto, ON: Webcom. ISBN 0-919115-76-4
  • Medline Plus

External Links


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